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米贝拉地尔在高血压长期治疗中的潜在心脏保护作用。

Potential cardioprotective effect of mibefradil in the long-term treatment of hypertension.

作者信息

Waeber B

机构信息

Division of Hypertension, CHUV, Lausanne, Switzerland.

出版信息

Cardiology. 1998;89 Suppl 1:16-22. doi: 10.1159/000047275.

Abstract

During the last 2 decades, remarkable progress has been made in the treatment of hypertension with the discovery of new drugs lowering blood pressure by various mechanisms, e.g. calcium channel blockers, angiotensin-converting enzyme inhibitors and angiotensin II antagonists. These antihypertensive agents are now widely used as first-line therapy although there is still no definite proof that they have a cardioprotective effect and reduce the mortality rate in patients with coronary heart disease. Mibefradil is a new calcium antagonist with a novel mechanism of action since it is the only drug available so far able to block T channels. This compound might be particularly effective in preventing cardiac morbidity and mortality. It reduces heart rate when lowering blood pressure, has no negative inotropic effect, allows regression of cardiac hypertrophy and is effective in the treatment of angina. Mibefradil produces a sustained blood pressure reduction with a close to optimal trough:peak ratio. A major advantage of this novel compound is its excellent tolerability over the dose range recommended (50-100 mg/day). In particular, leg edema is seen clearly less often during mibefradil treatment than during therapy with dihydropyridines. Mibefradil has therefore an attractive profile in terms of both efficacy and safety and represents a promising first-line option to treat hypertensive patients.

摘要

在过去20年里,高血压治疗取得了显著进展,发现了多种通过不同机制降低血压的新药,如钙通道阻滞剂、血管紧张素转换酶抑制剂和血管紧张素II拮抗剂。这些抗高血压药物目前被广泛用作一线治疗药物,尽管仍没有确凿证据表明它们具有心脏保护作用并能降低冠心病患者的死亡率。米贝拉地尔是一种新型钙拮抗剂,作用机制独特,因为它是目前唯一能够阻断T通道的药物。这种化合物在预防心脏发病和死亡方面可能特别有效。它在降低血压时能降低心率,没有负性肌力作用,可使心脏肥大消退,对心绞痛治疗有效。米贝拉地尔能持续降低血压,谷峰比接近最佳。这种新型化合物的一个主要优点是在推荐剂量范围(50 - 100毫克/天)内耐受性极佳。特别是,与二氢吡啶类药物治疗相比,米贝拉地尔治疗期间腿部水肿的发生率明显更低。因此,米贝拉地尔在疗效和安全性方面都具有吸引力,是治疗高血压患者的一个有前景的一线选择。

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